LatestDomestic BTK inhibitor declaration status, development progress, clinical trial information summary

- Jul 17, 2018-

Bruton's tyrosine kinase (BTK) is an important signaling molecule of B cell receptor pathway, which is expressed in various developmental stages of B lymphocytes and participates in the regulation of B cell proliferation, differentiation and apoptosis in malignant B. It plays an important role in the survival and spread of cells, and is currently a research hotspot in the clinical research of B cell tumors and B cell immune diseases.4255-62-3


Ibrutinib is the only listed BTK inhibitor in the world. It was approved by the FDA in November 2013. The current market indications include chronic lymphocytic leukemia, small lymphocytic lymphoma, mantle cell lymphoma, Waldenström macroglobulin blood. disease. In 2016, Ibrutini has global sales of more than $3 billion and is the world's best-selling leukemia drug.

Progress in the development of BTK inhibitors abroad



BTK inhibitor small molecule targeting drugs provide a new way for the treatment of B cell malignant tumors and some B cell immune diseases. The single-agent clinical treatment of the already marketed BTK inhibitor, ibrutinib, is exciting. However, ibrutinib has problems such as low oral availability, high plasma protein binding rate, and long-term drug safety (bleeding, myelosuppression, nephrotoxicity, etc.).



At present, a series of inhibitors targeting BTK are in the pre-clinical development or clinical trial stage, in order to obtain more efficient and low-toxic drugs, further prolong the survival time of patients and improve the quality of life. Among the research molecules, in addition to Baekje Shenzhou's BGB-3111, AstraZeneca's Acalabrutinib has also entered Phase III clinical.



Acalabrutinib is a highly selective, irreversible, second-generation BTK inhibitor that blocks the BTK pathway more selectively without disrupting other molecular pathways important for platelet and immune function, thereby avoiding or reducing cancer therapy The generation of related side effects. The drug is currently in Phase III clinical use for chronic lymphocytic leukemia.

Acalabrutinib was developed by Acerta. At the end of 2015, AZ acquired a 55% stake in Acerta for $4 billion to acquire the drug. In a Phase I/II clinical study of patients with recurrent chronic lymphocytes, patients receiving Acalabrutinib had a total response rate of 95% after an average follow-up of 14.3 months, and the remaining 5% were stable. In patients with a 17p13.1 deletion, the overall response rate was 100%. The most common adverse events were headache (43%), diarrhea (39%), and weight gain (26%), and most adverse events were grade 1 or 2.

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